CA2464214C - Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees - Google Patents

Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees Download PDF

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CA2464214C
CA2464214C CA2464214A CA2464214A CA2464214C CA 2464214 C CA2464214 C CA 2464214C CA 2464214 A CA2464214 A CA 2464214A CA 2464214 A CA2464214 A CA 2464214A CA 2464214 C CA2464214 C CA 2464214C
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inhibitors
src
inhibitor
day
protein
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CA2464214A1 (fr
Inventor
David G. Hangauer, Jr.
Moustafa E. El-Araby
Karen L. Milkiewicz
Thomas Nicotera
Donald Henderson
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Park Roswell Cancer Institute
Research Foundation of the State University of New York
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Park Roswell Cancer Institute
Research Foundation of the State University of New York
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

La présente invention concerne une méthode d'identification d'inhibiteurs de protéines kinases et/ou de protéines phosphatases. Cette invention concerne également des méthodes permettant d'inhiber l'activité des protéines kinases et/ou des protéines phosphatases. Cette invention porte en outre sur des inhibiteurs non peptidiques spécifiques de protéines tyrosines kinases et/ou de protéines phosphatases. Les inhibiteurs de protéines kinases ou de protéines phosphatases de la présente invention peuvent être utilisés pour traiter un certain nombre d'états chez des patients, tels que le cancer, le psoriasis, l'arthrosclérose, des troubles de l'activité du système immunitaire, le diabète ou l'obésité. En outre, cette invention porte sur une méthode de prévention ou de traitement de la perte auditive chez un sujet. Cette méthode consiste à administrer au sujet une quantité efficace d'un inhibiteur de protéines tyrosines kinases aux fins de la prévention ou du traitement de la perte auditive.
CA2464214A 2001-10-22 2002-10-19 Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees Expired - Fee Related CA2464214C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33619101P 2001-10-22 2001-10-22
US60/336,191 2001-10-22
US41072602P 2002-09-13 2002-09-13
US60/410,726 2002-09-13
PCT/US2002/033660 WO2003035621A1 (fr) 2001-10-22 2002-10-19 Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees

Publications (2)

Publication Number Publication Date
CA2464214A1 CA2464214A1 (fr) 2003-05-01
CA2464214C true CA2464214C (fr) 2011-02-08

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CA2464214A Expired - Fee Related CA2464214C (fr) 2001-10-22 2002-10-19 Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees

Country Status (6)

Country Link
US (2) US7129225B2 (fr)
EP (1) EP1444204A4 (fr)
JP (2) JP4623962B2 (fr)
CA (1) CA2464214C (fr)
MX (1) MXPA04003758A (fr)
WO (1) WO2003035621A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE494388T1 (de) 1999-01-13 2011-01-15 Univ New York State Res Found Neues verfahren zum erschaffen von proteinkinase- inhibitoren
CA2464214C (fr) 2001-10-22 2011-02-08 The Research Foundation Of State University Of New York Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees
US7005445B2 (en) 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
AU2003231370A1 (en) 2002-04-18 2003-10-27 Institute Of Medicinal Molecular Design. Inc. Amide derivatives
WO2004014851A2 (fr) 2002-08-09 2004-02-19 Merck & Co., Inc. Inhibiteurs de tyrosine kinases
US20060128783A1 (en) * 2002-08-09 2006-06-15 Dinsmore Christopher J Tyrosine kinase inhibitors
WO2004055154A2 (fr) * 2002-12-17 2004-07-01 Centre National De La Recherche Scientifique (Cnrs) Technique permettant d'induire la differentiation de cellules pileuses surnumeraires et de cellules de deiter dans l'organe de corti en developpement
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
EP1643991B1 (fr) * 2003-07-11 2014-03-12 Merck Patent GmbH Benzimidazole carboxamides utilises en tant qu'inhibiteurs de la kinase raf
US20050089936A1 (en) * 2003-10-23 2005-04-28 Jianping Cai Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid amides
EP1532980A1 (fr) 2003-11-24 2005-05-25 Novo Nordisk A/S Carboxamides d'indole n-heteroarylé et leurs analogues, utiles comme des activateurs de glucokinase pour le traitement de diabetes
WO2005114197A2 (fr) * 2004-04-15 2005-12-01 Albert Einstein College Of Medicine Of Yeshiva University Sondes à activité pour les protéines tyrosine phosphatase
WO2006053274A2 (fr) 2004-11-15 2006-05-18 Bristol-Myers Squibb Company Derives de tetraline 2-amino-1-fonctionnalises et inhibiteurs correspondants de glycogene phosphorylase
WO2006055462A1 (fr) 2004-11-15 2006-05-26 Bristol-Myers Squibb Company Derives 2-amino-4- tetraline fonctionnalisee et inhibiteurs de la glycogene phosphorylase associes
US7223786B2 (en) * 2004-11-15 2007-05-29 Bristol-Myers Squibb Company 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
WO2006055463A2 (fr) 2004-11-15 2006-05-26 Bristol-Myers Squibb Company Derives de 2-amino-3-tetraline fonctionnalisee et inhibiteurs de la glycogene phosphorylase associes
GB0425919D0 (en) * 2004-11-25 2004-12-29 Prosidion Ltd Indole-2-carboxylic acid amides
EA012613B1 (ru) * 2004-12-06 2009-10-30 Авентис Фарма С.А. Замещённые индолы, содержащие их композиции, способ получения и применение
FR2878849B1 (fr) 2004-12-06 2008-09-12 Aventis Pharma Sa Indoles substitues, compositions les contenant, procede de fabrication et utilisation
KR20070092297A (ko) * 2004-12-21 2007-09-12 데브젠 엔브이 Ｋｖ4 이온 채널 활성을 갖는 화합물
JP5094394B2 (ja) * 2005-04-20 2012-12-12 武田薬品工業株式会社 縮合複素環化合物
FR2884821B1 (fr) * 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
MY148644A (en) 2005-07-18 2013-05-15 Orion Corp New pharmaceutical compounds
EP1966150A4 (fr) * 2005-12-23 2011-07-20 Astrazeneca Ab Pyrazoles pour le traitement du rgop et du sii
US7838542B2 (en) 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
EP2069302B1 (fr) 2006-09-15 2010-08-25 Pfizer Inc. Composés de pyridiylméthyle bicyclocarboxyamide substitué
CA2666539A1 (fr) 2006-10-23 2008-05-02 Pfizer Inc. Composes de phenylmethyl bicyclocarboxyamide substitues
JP2010510202A (ja) 2006-11-17 2010-04-02 ファイザー株式会社 置換ビシクロカルボキシアミド化合物
WO2008077079A1 (fr) * 2006-12-18 2008-06-26 Ambrx, Inc. Compositions renfermant des acides aminés non naturels et polypeptides, procédés impliquant lesdits acides aminés non naturels et polypeptides et utilisations de ces derniers
JP2010523652A (ja) 2007-04-13 2010-07-15 エージェンシー フォー サイエンス，テクノロジー アンド リサーチ 腫瘍発生を制御する方法および腫瘍発生のリスクを診断する方法
CN101808995A (zh) 2007-07-27 2010-08-18 百时美施贵宝公司 新颖的葡糖激酶激活剂及其使用方法
CN101821253B (zh) 2007-08-31 2013-07-17 安斯泰来制药有限公司 哌啶衍生物
CN101945656B (zh) * 2008-02-19 2014-06-11 帝斯曼知识产权资产管理有限公司 3，3＇-二吲哚基甲烷的新颖用途
CN102105133B (zh) 2008-07-21 2015-06-17 奥德纳米有限公司 控制释放型耳结构调节和先天性免疫系统调节组合物以及治疗耳部病症的方法
PE20110303A1 (es) 2008-09-11 2011-05-21 Pfizer Derivados de heteroaril acetamidas como activadores de glucoquinasa
ES2427279T3 (es) 2009-03-11 2013-10-29 Pfizer Inc. Derivados de benzofuranilo usados como inhibidores de glucocinasa
WO2014037900A1 (fr) 2012-09-07 2014-03-13 Novartis Ag Dérivés d'indole carboxamide et leurs utilisations
CN103044311B (zh) * 2012-12-26 2015-04-22 山东大学 一种多取代吲哚类化合物及其制备方法和应用
ES2823825T3 (es) * 2014-04-04 2021-05-10 Iomet Pharma Ltd Derivados de indol para su uso en medicina
CN104876851A (zh) * 2015-05-15 2015-09-02 南京大学 一类含吲哚-3羧酸骨架的哌嗪类衍生物的制备方法及在抗癌药物中的应用
PT3426243T (pt) 2016-03-09 2021-08-19 Raze Therapeutics Inc Inibidores de 3-fosfoglicerato desidrogenase e utilizações dos mesmos
EP3426244B1 (fr) 2016-03-09 2023-06-07 Raze Therapeutics, Inc. Inhibiteurs de la 3-phosphoglycérate déshydrogénase et leurs utilisations
SG11202007143UA (en) 2018-01-31 2020-08-28 Heparegenix Gmbh Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2019243315A1 (fr) 2018-06-21 2019-12-26 Heparegenix Gmbh Inhibiteurs de protéine kinase tricycliques pour favoriser la régénération du foie ou réduire ou prévenir la mort des hépatocytes
IL279641B2 (en) 2018-07-16 2024-04-01 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
JP7639008B2 (ja) 2020-01-15 2025-03-04 ヘパリジェニックス ゲーエムベーハー 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤
US20230183810A1 (en) * 2020-05-04 2023-06-15 Dna-Seq, Inc. Methods and systems for determination of an effective therapeutic regimen and drug discovery
WO2022020114A2 (fr) 2020-07-10 2022-01-27 Ting Therapeutics Llc Méthodes de prévention et de traitement de la perte d'audition
WO2024109642A1 (fr) * 2023-07-28 2024-05-30 常州大学 UTILISATION D'UN COMPOSÉ BENZOAZACYCLIQUE EN TANT QUE MODULATEUR ALLOSTÉRIQUE D'UN β2-ADRÉNORÉCEPTEUR

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01132579A (ja) * 1987-11-19 1989-05-25 Ss Pharmaceut Co Ltd インドール誘導体
GB8827189D0 (en) 1988-11-21 1988-12-29 Fujisawa Pharmaceutical Co 2(1h)-quinolinone compounds processes for preparation thereof & pharmaceutical composition comprising same
CA2071529C (fr) * 1989-12-28 2001-03-20 Donna Lee Romero Composes diaromatiques substitues contre le sida
US5552534A (en) * 1991-08-22 1996-09-03 The Trustees Of The University Of Pennsylvania Non-Peptide peptidomimetics
DE4307883A1 (en) 1992-03-12 1993-09-23 Westarp Martin Egon Dr Med Use of anti-retroviral substances - to treat motor-neuronal diseases
US5705585A (en) * 1993-06-30 1998-01-06 Arqule, Inc. Aminimide-containing molecules and materials as molecular recognition agents
CA2140440A1 (fr) * 1992-08-06 1994-02-17 Ellen M. Dobrusin 2-thioindoles (selenoindoles) et disulfides appparentes (selenides) qui inhibent les proteine-tyrosine-kinases et qui ont des proprietes antitumorales
US6011175A (en) * 1993-05-18 2000-01-04 University Of Pittsburgh Inhibition of farnesyltransferase
US5532167A (en) * 1994-01-07 1996-07-02 Beth Israel Hospital Substrate specificity of protein kinases
US5712171A (en) * 1995-01-20 1998-01-27 Arqule, Inc. Method of generating a plurality of chemical compounds in a spatially arranged array
FR2733995B1 (fr) 1995-05-09 1997-07-25 Inst Nat Sante Rech Med Inhibiteurs de l'inactivation de neuropeptides endogenes notamment la cholecystokinine, leurs procedes de preparation leur utilisation comme medicaments et procede de criblage de medicaments
JP3314938B2 (ja) * 1995-06-06 2002-08-19 ファイザー・インコーポレーテッド グリコーゲンホスホリラーゼ抑制剤としての置換されたｎ−（インドール−２−カルボニル）−グリシンアミド類および誘導体
FI974437A0 (fi) * 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogeenifosforylaasi-inhibiittoreina
US5648378A (en) * 1995-06-07 1997-07-15 Research Corporation Technologies, Inc. 2-iminochromene derivatives as inhibitors of protein tyrosine kinase
WO1997011692A2 (fr) * 1995-09-11 1997-04-03 Osteoarthritis Sciences, Inc. Inhibiteurs de proteine-tyrosine-kinase pour le traitement de l'osteo-arthrite
JP2001506230A (ja) * 1996-08-09 2001-05-15 スミスクライン・ビーチャム・コーポレイション 新規ピペラジン含有化合物
US5952322A (en) * 1996-12-05 1999-09-14 Pfizer Inc. Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
WO1998027108A2 (fr) * 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. Nouveaux composes amide
EP0974584B1 (fr) * 1997-02-21 2003-01-15 Takeda Chemical Industries, Ltd. Composes a anneaux condenses, leur procede de production et leur utilisation
US6420338B1 (en) * 1997-06-13 2002-07-16 New York University Medical Center Inhibition of the Src kinase family pathway as a method of treating HBV infection and hepatocellular carcinoma
GB9718913D0 (en) * 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
ATE293102T1 (de) * 1998-04-23 2005-04-15 Takeda Pharmaceutical Naphthalene derivate ,ihre herstellung und verwendung
WO1999059973A1 (fr) * 1998-05-15 1999-11-25 Guilford Pharmaceuticals Inc. Composes de carboxamide, compositions et methodes d'inhibition de l'activite de type poly(adp-ribose) polymerase (parp)
CN1329034C (zh) * 1998-09-25 2007-08-01 赛福伦公司 预防/治疗感觉毛细胞和耳蜗神经元损伤的药物
US7070936B1 (en) * 1999-01-13 2006-07-04 The Research Foundation Of State University Of New York Method for designing protein kinase inhibitors
ATE494388T1 (de) 1999-01-13 2011-01-15 Univ New York State Res Found Neues verfahren zum erschaffen von proteinkinase- inhibitoren
CA2382789A1 (fr) * 1999-08-27 2001-03-08 Sugen, Inc. Mimetiques phosphates et procedes de traitement utilisant des inhibiteurs de phosphatase
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
HN2001000008A (es) * 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
AU2868601A (en) * 2000-01-27 2001-08-07 Ribotargets Ltd Biaryl compounds, their preparation and their use in therapy
AR034118A1 (es) * 2000-02-15 2004-02-04 Sugen Inc Compuestos de 2-indolinonas sustituidas con pirroles inhibidoras de proteinquinasas; sus composiciones farmaceuticas e intermediarios de sintesis
KR100423899B1 (ko) 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
EA006153B1 (ru) * 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
ATE321052T1 (de) * 2000-07-07 2006-04-15 Novo Nordisk As Modulatoren von protein tyrosin phosphatasen (ptpasen)
AU2002336273A1 (en) 2001-03-09 2002-09-24 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
KR100429841B1 (ko) 2001-07-19 2004-05-04 삼성전자주식회사 Ｇｒｉｎ 렌즈를 구비하는 광 기록헤드
US7005445B2 (en) 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
CA2464214C (fr) * 2001-10-22 2011-02-08 The Research Foundation Of State University Of New York Inhibiteurs de proteines kinases et de proteines phosphatases, methodes d'identification et methodes d'utilisation associees
JP3975272B2 (ja) 2002-02-21 2007-09-12 独立行政法人産業技術総合研究所 超微細流体ジェット装置
CA2484209C (fr) 2002-05-03 2013-06-11 Exelixis, Inc. Modulateurs de proteine kinase et procedes d'utilisation
JP4539538B2 (ja) * 2005-11-17 2010-09-08 トヨタ自動車株式会社 エネルギ回収装置
US7838542B2 (en) 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

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US20040019015A1 (en) 2004-01-29
MXPA04003758A (es) 2005-06-20
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WO2003035621A1 (fr) 2003-05-01
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US20060172971A1 (en) 2006-08-03
US7129225B2 (en) 2006-10-31
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